Pharmaceutical composition for use as a contraceptive
DC CAFC
First Claim
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1. A pharmaceutical composition comprising from about 2 mg to about 4 mg of micronized drospirenone particles, about 0.01 mg to about 0.05 mg of 17α
- -ethinylestradiol, and one or more pharmaceutically acceptable carriers, the composition being in an oral dose form exposed to the gastric environment upon dissolution, and the composition being effective for oral contraception in a human female.
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Abstract
A pharmaceutical composition comprises, as a first active agent, 6β,7β;15β,16β-dimethylene-3-oxo-17α-pregn-4-ene-21,17-carbolactone (drospirenone) in an amount corresponding to a daily dosage, on administration of the composition, of from about 2 mg to about 4 mg, and, as a second active agent, 17α-ethinylestradiol (ethinylestradiol) in an amount corresponding to a daily dosage of from about 0.01 mg to about 0.05 mg, together with one or more pharmaceutically acceptable carriers or excipients.
In a specific embodiment, the composition consists of a number of separately packaged and individually removable daily dosage units placed in a packaging unit and intended for oral administration for a period of at least 21 consecutive days, wherein said daily dosage units comprises the combination of drospirenone and ethinylestradiol. The composition may further comprise 7 or less daily dosage units containing no active agent or containing ethinylestradiol alone.
78 Citations
52 Claims
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1. A pharmaceutical composition comprising from about 2 mg to about 4 mg of micronized drospirenone particles, about 0.01 mg to about 0.05 mg of 17α
- -ethinylestradiol, and one or more pharmaceutically acceptable carriers, the composition being in an oral dose form exposed to the gastric environment upon dissolution, and the composition being effective for oral contraception in a human female.
- View Dependent Claims (2, 3, 4, 5, 6, 7, 19, 20, 21, 26, 45, 46, 47, 51)
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8. A pharmaceutical kit comprising a number of separately packaged, individually removable, daily dosage units, in an oral dose form exposed to the gastric environment upon dissolution, placed in a packaging unit and intended for oral administration for a period of 21 consecutive days, wherein said daily dosage units each comprise a combination of micronized drospirenone particles in an amount of from about 2 mg to about 4 mg and 17α
- -ethinylestradiol in an amount from about 0.01 to about 0.05 mg, and wherein said daily dosage units comprising drospirenone are effective for oral contraception in a human female.
- View Dependent Claims (9, 13, 14, 16, 22, 24)
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10. A pharmaceutical kit comprising a number of separately packaged, individually removable, daily dosage units, in an oral dose form exposed to the gastric environment upon dissolution, placed in a packaging unit and intended for oral administration for a period of 22, 23 or 24 consecutive days, wherein said daily dosage units each comprise a combination of micronized drospirenone particles in an amount of from about 2 mg to about 4 mg and 17α
- -ethinylestradiol in an amount from about 0.01 to about 0.05 mg, and a number of daily dosage units containing no active agent which is 6, 5 or 4, and wherein said daily dosage units comprising drospirenone are effective for oral contraception in a human female.
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11. A pharmaceutical kit comprising a number of separately packaged, individually removable, daily dosage units, in an oral dose form exposed to the gastric environment upon dissolution, placed in a packaging unit and intended for oral administration for a period of 28, or a multiple of 28, consecutive days, wherein said daily dosage units each comprise a combination of micronized drospirenone particles in an amount of from about 2 mg to about 4 mg and 17α
- -ethinylestradiol in an amount from about 0.01 to about 0.05 mg, and wherein said daily dosage units comprising drospirenone are effective for oral contraception in a human female.
- View Dependent Claims (12, 52)
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15. A pharmaceutical kit comprising a number of separately packaged, individually removable, daily dosage units, in an oral dose form exposed to the gastric environment upon dissolution, placed in a packaging unit and intended for oral administration for a period of at least 28 consecutive days, wherein at least 21 of said daily dosage units comprise a combination of micronized drospirenone particles in an amount of from about 2 mg to about 4 mg and 17α
- -ethinylestradiol in an amount from about 0.01 to about 0.05 mg, wherein at least 1 but no more than 7 of said daily dosage units contain 17α
-ethinylestradiol in an amount from about 0.01 to about 0.05 mg and contain no drospirenone, and wherein said daily dosage units comprising drospirenone are effective for oral contraception in a human female. - View Dependent Claims (17, 18, 23, 25, 48)
- -ethinylestradiol in an amount from about 0.01 to about 0.05 mg, wherein at least 1 but no more than 7 of said daily dosage units contain 17α
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27. A pharmaceutical composition comprising:
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from about 2 mg to about 4 mg of drospirenone particles, wherein the drospirenone has a surface area of more than 10 000 cm2/g, about 0.01 to about 0.05 mg of 17α
-ethinylestradiol, andone or more pharmaceutically acceptable carriers, the composition being in an oral dose form exposed to the gastric environment upon dissolution, and the composition being effective for oral contraception in a human female. - View Dependent Claims (34, 35, 36, 37, 38, 39, 44)
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28. A pharmaceutical composition comprising:
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from about 2 mg to about 4 mg of drospirenone particles, wherein the drospirenone is in a form, which when provided in a tablet containing 3 mg of drospirenone, has a dissolution such that at least 70% of said drospirenone is dissolved in 900 ml of water at 37°
C. (±
0.5°
C.) within 30 minutes, as determined by USP XXIII Paddle Method using a USP dissolution test apparatus 2 at a stirring rate of 50 rpm, including 6 covered glass vessels and 6 paddles,about 0.01 mg to about 0.05 mg of 17α
-ethinylestradiol, andone or more pharmaceutically acceptable carriers, the composition being in an oral dose form exposed to the gastric environment upon dissolution, and the composition being effective for oral contraception in a human female. - View Dependent Claims (33)
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29. A pharmaceutical kit comprising a number of separately packaged, individually removable, daily dosage units, in an oral dose form exposed to the gastric environment upon dissolution, placed in a packaging unit and intended for oral administration for a period of 21 consecutive days, wherein said daily dosage units each comprise a combination of
drospirenone particles in an amount of from about 2 mg to about 4 mg, wherein the drospirenone has a surface area of more than 10 000 cm2/g, and 17α - -ethinylestradiol in an amount from about 0.01 to about 0.05 mg, and
wherein said daily dosage units comprising drospirenone are effective for oral contraception in a human female.
- -ethinylestradiol in an amount from about 0.01 to about 0.05 mg, and
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30. A pharmaceutical kit comprising a number of separately packaged, individually removable, daily dosage units, in an oral dose form exposed to the gastric environment upon dissolution, in a packaging unit and intended for oral administration for a period of 21 consecutive days, wherein said daily dosage units each comprise a combination of:
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drospirenone particles in an amount of from about 2 mg to about 4 mg, wherein the drospirenone is in a form, which when provided in a tablet containing 3 mg of drospirenone, has a dissolution such that at least 70% of said drospirenone is dissolved in 900 ml of water at 37°
C. (±
0.5°
C.) within 30 minutes, as determined by USP XXIII Paddle Method using a USP dissolution test apparatus 2 at a stirring rate of 50 rpm, including 6 covered glass vessels and 6 paddles, and17α
-ethinylestradiol in an amount from about 0.01 to about 0.05 mg, andwherein said daily dosage units comprising drospirenone are effective for oral contraception in a human female.
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31. A pharmaceutical kit comprising a number of separately packaged, individually removable, daily dosage units, in an oral dose form exposed to the gastric environment upon dissolution, in a packaging unit and intended for oral administration for a period of at least 28 consecutive days,
wherein at least 21 of said daily dosage units comprise a combination of: -
drospirenone particles in an amount of from about 2 mg to about 4 mg, wherein the drospirenone has a surface area of more than 10 000 cm2/g, and 17α
-ethinylestradiol in an amount from about 0.01 to about 0.05 mg, andwherein at least 1 but no more than 7 of said daily dosage units contain 17α
-ethinylestradiol in an amount from about 0.01 to about 0.05 mg and contain no drospirenone, andwherein said daily dosage units comprising drospirenone are effective for oral contraception in a human female.
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32. A pharmaceutical kit comprising a number of separately packaged, individually removable, daily dosage units, in an oral dose form exposed to the gastric environment upon dissolution, in a packaging unit and intended for oral administration for a period of at least 28 consecutive days,
wherein at least 21 of said daily dosage units comprise a combination of drospirenone particles in an amount of from about 2 mg to about 4 mg, wherein the drospirenone is in a form, which when provided in a tablet containing 3 mg of drospirenone, has a dissolution such that at least 70% of said drospirenone is dissolved in 900 ml of water at 37° - C. (±
0.5°
C.) within 30 minutes, as determined by USP XXIII Paddle Method using a USP dissolution test apparatus 2 at a stirring rate of 50 rpm, including 6 covered glass vessels and 6 paddles, and17α
-ethinylestradiol in an amount from about 0.01 to about 0.05 mg, andwherein at least 1 but no more than 7 of said daily dosage units contain 17α
-ethinylestradiol in an amount from about 0.01 to about 0.05 mg and contain no drospirenone, andwherein said daily dosage units comprising drospirenone are effective for oral contraception in a human female.
- C. (±
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40. A pharmaceutical kit comprising a number of separately packaged, individually removable, daily dosage units, in an oral dose form exposed to the gastric environment upon dissolution, in a packaging unit, including active daily dosage units which comprise a combination of micronized drospirenone particles in an amount of from about 2 mg to about 4 mg and 17α
- -ethinylestradiol in an amount from about 0.01 to about 0.05 mg, wherein the kit is adapted for administering active daily dosage units for multiple cycles of 28 consecutive days each, followed by administering the active daily dosage units for 21, 22, 23 or 24 consecutive days and subsequently administering daily dosage units containing no active agent, or administering no daily dosage units, for 7, 6, 5 or 4 consecutive days, and wherein said daily dosage units comprising drospirenone are effective for oral contraception in a human female.
- View Dependent Claims (43)
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41. A pharmaceutical kit comprising a number of separately packaged, individually removable, daily dosage units, in an oral dose form exposed to the gastric environment upon dissolution, in a packaging unit, including active daily dosage units which comprise a combination of:
-
drospirenone particles in an amount of from about 2 mg to about 4 mg, wherein the drospirenone is in a form, which when provided in a tablet containing 3 mg of drospirenone, has a dissolution such that at least 70% of said drospirenone is dissolved in 900 ml of water at 37°
C. (±
0.5°
C.) within 30 minutes, as determined by USP XXIII Paddle Method using a USP dissolution test apparatus 2 at a stirring rate of 50 rpm, including 6 covered glass vessels and 6 paddles, and17α
-ethinylestradiol in an amount from about 0.01 to about 0.05 mg,wherein the kit is adapted for administering active daily dosage units for multiple cycles of 28 consecutive days each, followed by administering active daily dosage units for 21, 22, 23 or 24 consecutive days and subsequently administering daily dosage units containing no active agent, or administering no daily dosage units, for 7, 6, 5 or 4 consecutive days, and wherein said daily dosage units comprising drospirenone are effective for oral contraception in a human female.
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42. A pharmaceutical kit comprising a number of separately packaged, individually removable, daily dosage units, in an oral dose form exposed to the gastric environment upon dissolution, in a packaging unit, including active daily dosage units which comprise a combination of:
-
drospirenone particles in an amount of from about 2 mg to about 4 mg, wherein the drospirenone has a surface area of more than 10 000 cm2/g, and 17α
-ethinylestradiol in an amount from about 0.01 to about 0.05 mg,wherein the kit is adapted for administering active daily dosage units for multiple cycles of 28 consecutive days each, followed by administering active daily dosage units for 21, 22, 23 or 24 consecutive days and subsequently administering daily dosage units containing no active agent, or administering no daily dosage units, for 7, 6, 5 or 4 consecutive days, and wherein said daily dosage units comprising drospirenone are effective for oral contraception in a human female.
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49. A pharmaceutical composition comprising about 3 mg of micronized drospirenone particles, about 0.03 mg of micronized 17α
- -ethinylestradiol, and one or more pharmaceutically acceptable carriers, the composition being in a tablet, capsule or pill oral dose exposed to the gastric environment upon dissolution, and the composition being effective for oral contraception in a human female.
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50. A pharmaceutical kit comprising a number of separately packaged, individually removable, daily dosage units, in an oral dose form exposed to the gastric environment upon dissolution, placed in a packaging unit and intended for oral administration for a period of 28 consecutive days, wherein 21 of said daily dosage units comprise a combination of micronized drospirenone particles in an amount of about 3 mg and micronized 17α
- -ethinylestradiol in an amount of about 0.03 mg, and wherein 7 of said daily dosage units contain no drospirenone or 17α
-ethinylestradiol, andwherein said daily dosage units comprising drospirenone are effective for oral contraception in a human female.
- -ethinylestradiol in an amount of about 0.03 mg, and wherein 7 of said daily dosage units contain no drospirenone or 17α
Specification
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Litigation Data
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Current AssigneeBayer Schering Pharma AG (Bayer AG)
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Original AssigneeSchering Ag (Merck & Co., Inc.)
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InventorsTack, Johannes W., Heil, Wolfgang, Lipp, Ralph, Huempel, Michael, Hilman, Juergen, Heithecker, Renate
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Primary Examiner(s)Hui, San Ming R.
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Application NumberUS09/654,227Time in Patent Office1,468 DaysField of Search514/171, 514/178, 514/181US Class Current514/171CPC Class CodesA61K 2300/00 Mixtures or combinations of...A61K 31/56 Compounds containing cyclop...A61K 31/567 substituted in position 17 ...A61K 31/585 containing lactone rings, e...
